Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators

Whereas the PROTAC approach to target protein degradation greatly benefits from rational design, the discovery of small-molecule degraders relies mostly on phenotypic screening and retrospective target identification efforts. Here, we describe the design, synthesis, and screening of a large diverse...

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Bibliographic Details

Published in:	Journal of medicinal chemistry Vol. 64; no. 11; p. 7296
Main Authors:	Nishiguchi, Gisele, Keramatnia, Fatemeh, Min, Jaeki, Chang, Yunchao, Jonchere, Barbara, Das, Sourav, Actis, Marisa, Price, Jeanine, Chepyala, Divyabharathi, Young, Brandon, McGowan, Kevin, Slavish, P Jake, Mayasundari, Anand, Jarusiewicz, Jamie A, Yang, Lei, Li, Yong, Fu, Xiang, Garrett, Shalandus H, Papizan, James B, Kodali, Kiran, Peng, Junmin, Pruett Miller, Shondra M, Roussel, Martine F, Mullighan, Charles, Fischer, Marcus, Rankovic, Zoran
Format:	Journal Article
Language:	English
Published:	10.06.2021
ISSN:	1520-4804, 1520-4804
Online Access:	Get more information
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